IL178674A0 - PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PYRIMIDINE ADENOSINE A2A RECEPTOR ANTAGONISTS - Google Patents
PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PYRIMIDINE ADENOSINE A2A RECEPTOR ANTAGONISTSInfo
- Publication number
- IL178674A0 IL178674A0 IL178674A IL17867406A IL178674A0 IL 178674 A0 IL178674 A0 IL 178674A0 IL 178674 A IL178674 A IL 178674A IL 17867406 A IL17867406 A IL 17867406A IL 178674 A0 IL178674 A0 IL 178674A0
- Authority
- IL
- Israel
- Prior art keywords
- triazolo
- pyrazolo
- receptor antagonists
- pyrimidine adenosine
- adenosine
- Prior art date
Links
- 229940123702 Adenosine A2a receptor antagonist Drugs 0.000 title 1
- NJAKSMOWBFDNNW-MCDZGGTQSA-N N1=CN2NC=NC2=C2C=NN=C21.C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O Chemical compound N1=CN2NC=NC2=C2C=NN=C21.C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O NJAKSMOWBFDNNW-MCDZGGTQSA-N 0.000 title 1
- 239000002467 adenosine A2a receptor antagonist Substances 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US56391304P | 2004-04-21 | 2004-04-21 | |
| US60996604P | 2004-09-15 | 2004-09-15 | |
| PCT/US2005/013454 WO2005103055A1 (en) | 2004-04-21 | 2005-04-19 | PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PYRIMIDINE ADENOSINE A2A RECEPTOR ANTAGONISTS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL178674A0 true IL178674A0 (en) | 2007-02-11 |
Family
ID=34966464
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL178674A IL178674A0 (en) | 2004-04-21 | 2006-10-17 | PYRAZOLO-[4,3-e]-1,2,4-TRIAZOLO-[1,5-c]-PYRIMIDINE ADENOSINE A2A RECEPTOR ANTAGONISTS |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US7709492B2 (es) |
| EP (1) | EP1745047B1 (es) |
| JP (2) | JP2007533754A (es) |
| KR (1) | KR20060135901A (es) |
| AR (1) | AR048617A1 (es) |
| AT (1) | ATE461932T1 (es) |
| AU (1) | AU2005236059B2 (es) |
| CA (1) | CA2563635A1 (es) |
| DE (1) | DE602005020127D1 (es) |
| ES (1) | ES2342082T3 (es) |
| IL (1) | IL178674A0 (es) |
| MX (1) | MXPA06012231A (es) |
| NZ (1) | NZ550591A (es) |
| PE (1) | PE20060185A1 (es) |
| TW (1) | TW200538118A (es) |
| WO (1) | WO2005103055A1 (es) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SK287748B6 (sk) * | 2000-05-26 | 2011-08-04 | Schering Corporation | Substituované 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo[1,5- c]pyrimidíny, spôsob ich výroby, farmaceutický prostriedok s ich obsahom a ich použitie |
| US20060128694A1 (en) * | 2002-12-19 | 2006-06-15 | Michael Grzelak | Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders |
| DK1667964T3 (da) | 2003-09-19 | 2009-10-26 | Janssen Pharmaceutica Nv | 4-((Phenoxyalkyl)thio)-phenoxyeddikesyrer og analoger |
| MY147518A (en) | 2004-09-15 | 2012-12-31 | Janssen Pharmaceutica Nv | 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs |
| CA2588595A1 (en) * | 2004-12-13 | 2006-06-22 | Arena Pharmaceuticals, Inc. | N-biaryl and n-arylheteroaryl piperazine derivatives as modulators of the 5ht2c receptor useful for the treatment of disorders related thereto |
| EP1844792A4 (en) * | 2004-12-14 | 2008-05-21 | Shionogi & Co | THERAPEUTIC AGENT AGAINST OBSTIPATION |
| JO3006B1 (ar) | 2005-09-14 | 2016-09-05 | Janssen Pharmaceutica Nv | املاح ليسين مبتكرة من مشتقات حامض 4-((فينوكسي الكيل)ثيو) فينوكسي الخليك |
| WO2007035542A1 (en) * | 2005-09-19 | 2007-03-29 | Schering Corporation | 2-HETEROARYL-PYRAZOLO-[4, 3-e]-1, 2, 4-TRIAZOLO-[1,5-c]-PYRIMIDINE AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| PE20070521A1 (es) | 2005-09-23 | 2007-07-13 | Schering Corp | 7-[2-[4-(6-FLUORO-3-METIL-1,2-BENCISOXAZOL-5-IL)-1-PIPERAZINIL]ETIL]-2-(1-PROPINIL)-7H-PIRAZOL-[4,3-E]-[1,2,4]-TRIAZOL-[1,5-C]-PIRIMIDIN-5-AMINA COMO ANTAGONISTA DEL RECEPTOR DE ADENOSINA A2a |
| PE20080188A1 (es) | 2006-04-18 | 2008-03-10 | Janssen Pharmaceutica Nv | Derivados del acido benzoazepin-oxi-acetico como agonistas de ppar-delta usados para aumentar hdl-c, reducir ldl-c y reducir colesterol |
| US7723343B2 (en) | 2007-03-30 | 2010-05-25 | King Pharmaceuticals Research And Development, Inc. | Adenosine A2A receptor antagonists |
| AU2009222047A1 (en) | 2008-03-04 | 2009-09-11 | Schering Corporation | 1,2,4-triazolo[4,3-c]pyrimidin-3-one and pyrazolo [4,3-e] -1,2,4-triazolo [4,3-c] pyrimidin-3-one compounds for use as adenosine A2a receptor antagonists |
| US8153416B2 (en) | 2008-12-10 | 2012-04-10 | Thesis Chemistry, Llc | Process for manufacture of optically active 2-(acyloxymethyl)-1,3-oxathiolanes using enzymatic resolution |
| WO2010078430A1 (en) * | 2008-12-30 | 2010-07-08 | Arqule, Inc. | Substituted 1h-pyrazolo[3,4-d]pyrimidine-6-amine compounds |
| US8431699B2 (en) * | 2009-02-27 | 2013-04-30 | Vertichem Corporation | Method for manufacture of 2-oxoimidazolidines |
| BRPI1009252A2 (pt) | 2009-03-10 | 2016-03-15 | Takeda Pharmaceutical | composto, pró-droga, composição farmacêutica, métodos para prevenir ou tratar doenças do sistema nervoso central, e mal de alzheimer, e, uso do composto ou de uma pró-droga do mesmo |
| TW201100427A (en) * | 2009-03-31 | 2011-01-01 | Arqule Inc | Substituted heterocyclic compounds |
| EP2486024B1 (en) * | 2009-10-08 | 2015-04-22 | Sanofi | Phenyloxadiazole derivatives as pgds inhibitors |
| JP5843869B2 (ja) * | 2010-09-24 | 2016-01-13 | アドヴィナス・セラピューティックス・リミテッド | アデノシン受容体拮抗薬としての縮合三環化合物 |
| WO2012135084A1 (en) * | 2011-03-31 | 2012-10-04 | Merck Sharp & Dohme Corp. | METABOLITES OF 2-(FURAN-2-YL)-7-(2-(4-(4-(2-METHOXYETHOXY)PHENYL)PIPERAZIN-1-YL)ETHYL)-7H-PYRAZOLO[4,3-e][1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-5-AMINE AND THEIR UTILITY AS ADENOSINE A2a RECEPTOR ANTAGONISTS |
| ES2716832T3 (es) * | 2011-12-27 | 2019-06-17 | Bio Pharm Solutions Co Ltd | Compuestos carbamatos de fenilo para su uso en el alivio o el tratamiento del dolor y el dolor neuropático |
| WO2018178338A1 (en) * | 2017-03-30 | 2018-10-04 | Iteos Therapeutics | 2-oxo-thiazole derivatives as a2a inhibitors and compounds for use in the treatment of cancers |
| CA3058260A1 (en) * | 2017-03-30 | 2018-10-04 | Iteos Therapeutics | 2-oxo-thiazole derivatives as a2a inhibitors and compounds for use in the treatment of cancers |
| CN108148004A (zh) * | 2017-12-31 | 2018-06-12 | 佛山市赛维斯医药科技有限公司 | 一种含丙酰肼和嘧啶结构的化合物、制备方法及其用途 |
| CN107935953A (zh) * | 2017-12-31 | 2018-04-20 | 佛山市赛维斯医药科技有限公司 | 含末端烯键和酰肼结构的comt抑制剂、制备方法及其用途 |
| CN108191775A (zh) * | 2017-12-31 | 2018-06-22 | 佛山市赛维斯医药科技有限公司 | 一种末端烯丙基丙酰肼结构化合物及其用途 |
| CN108218796A (zh) * | 2017-12-31 | 2018-06-29 | 佛山市赛维斯医药科技有限公司 | 含酰肼结构的化合物、制备方法及其用途 |
| SG11202009706VA (en) | 2018-04-08 | 2020-10-29 | Beigene Ltd | Pyrazolotriazolopyrimidine derivatives as a2a receptor antagonist |
| CN110742893B (zh) * | 2018-07-23 | 2024-04-05 | 百济神州(北京)生物科技有限公司 | A2a受体拮抗剂治疗癌症的方法 |
| JP2022500496A (ja) * | 2018-09-11 | 2022-01-04 | アイテオ ベルギウム エスエー | A2a阻害剤としてのチオカルバメート誘導体、その医薬組成物、及び抗がん剤との組み合わせ |
| US11376255B2 (en) | 2018-09-11 | 2022-07-05 | iTeos Belgium SA | Thiocarbamate derivatives as A2A inhibitors, pharmaceutical composition thereof and combinations with anticancer agents |
| BE1026615B1 (fr) * | 2018-09-27 | 2020-07-06 | Iteos Therapeutics S A | Combinaison d’un inhibiteur du récepteur a2a et d'un agent anticancéreux |
| BE1026758B1 (fr) * | 2018-09-11 | 2020-06-09 | Iteos Therapeutics S A | Composition pharmaceutique comprenant des dérivés de thiocarbamate inhibiteurs d’a2a |
| US11427594B2 (en) | 2018-09-27 | 2022-08-30 | iTeos Belgium SA | Non brain penetrant A2A inhibitors and methods for use in the treatment of cancers |
| BE1026602B1 (fr) * | 2018-09-27 | 2020-06-18 | Iteos Therapeutics S A | Inhibiteurs d’a2a ne penetrant pas dans le cerveau et methodes d’utilisation dans le traitement de cancers |
| WO2020106558A1 (en) | 2018-11-20 | 2020-05-28 | Merck Sharp & Dohme Corp. | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| WO2020106560A1 (en) | 2018-11-20 | 2020-05-28 | Merck Sharp & Dohme Corp. | Substituted amino triazolopyrimidine and amino triazolopyrazine adenosine receptor antagonists, pharmaceutical compositions and their use |
| JP2022511778A (ja) | 2018-11-30 | 2022-02-01 | メルク・シャープ・アンド・ドーム・コーポレーション | アデノシン受容体拮抗薬としての7-、8-及び10-置換されたアミノトリアゾロキナゾリン誘導体、医薬組成物及びそれらの使用 |
| JOP20210116A1 (ar) | 2018-11-30 | 2023-01-30 | Merck Sharp & Dohme | مشتقات أمينو ترايازولو كوينازولين بها استبدال في الموضع-9 كمضادات مستقبل أدينوزين، تركيبات صيدلانية واستخدامها |
| WO2020227156A1 (en) * | 2019-05-03 | 2020-11-12 | Nektar Therapeutics | Adenosine 2 receptor antagonists |
| US20230024108A1 (en) * | 2019-07-17 | 2023-01-26 | Teon Therapeutics, Inc. | Adenosine a2a receptor antagonists |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1264901B1 (it) | 1993-06-29 | 1996-10-17 | Schering Plough S P A | Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina |
| ATE208199T1 (de) * | 1993-07-27 | 2001-11-15 | Kyowa Hakko Kogyo Kk | Arzneimittel gegen parkinsonsche krankheit |
| IT1277392B1 (it) | 1995-07-28 | 1997-11-10 | Schering Plough S P A | Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina |
| IT1291372B1 (it) | 1997-05-21 | 1999-01-07 | Schering Plough S P A | Uso di analoghi eterociclici di 1,2,4-triazolo (1,5-c) pirimidine per la preparazione di medicamenti utili per il trattamento delle malattie |
| SK287748B6 (sk) * | 2000-05-26 | 2011-08-04 | Schering Corporation | Substituované 5-amino-pyrazolo[4,3-e]-1,2,4-triazolo[1,5- c]pyrimidíny, spôsob ich výroby, farmaceutický prostriedok s ich obsahom a ich použitie |
| GB0100624D0 (en) | 2001-01-10 | 2001-02-21 | Vernalis Res Ltd | Chemical compounds VII |
| EP1435960B1 (en) | 2001-10-15 | 2014-07-30 | Merck Sharp & Dohme Corp. | Imidazo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as adenosine a2a receptor antagonists |
| NZ540493A (en) | 2002-12-19 | 2008-04-30 | Schering Corp | Uses of adenosine A2a receptor antagonists |
| TWI355381B (en) * | 2003-04-23 | 2012-01-01 | Schering Corp | 2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-tri |
-
2005
- 2005-04-19 AT AT05737774T patent/ATE461932T1/de not_active IP Right Cessation
- 2005-04-19 CA CA002563635A patent/CA2563635A1/en not_active Abandoned
- 2005-04-19 PE PE2005000428A patent/PE20060185A1/es not_active Application Discontinuation
- 2005-04-19 DE DE602005020127T patent/DE602005020127D1/de not_active Expired - Lifetime
- 2005-04-19 MX MXPA06012231A patent/MXPA06012231A/es active IP Right Grant
- 2005-04-19 EP EP05737774A patent/EP1745047B1/en not_active Expired - Lifetime
- 2005-04-19 JP JP2007509594A patent/JP2007533754A/ja active Pending
- 2005-04-19 US US11/108,916 patent/US7709492B2/en active Active
- 2005-04-19 NZ NZ550591A patent/NZ550591A/en unknown
- 2005-04-19 WO PCT/US2005/013454 patent/WO2005103055A1/en not_active Ceased
- 2005-04-19 AU AU2005236059A patent/AU2005236059B2/en not_active Ceased
- 2005-04-19 ES ES05737774T patent/ES2342082T3/es not_active Expired - Lifetime
- 2005-04-19 TW TW094112339A patent/TW200538118A/zh unknown
- 2005-04-19 KR KR1020067021803A patent/KR20060135901A/ko not_active Ceased
- 2005-04-20 AR ARP050101559A patent/AR048617A1/es not_active Application Discontinuation
-
2006
- 2006-10-17 IL IL178674A patent/IL178674A0/en unknown
-
2008
- 2008-04-08 JP JP2008100773A patent/JP2008231111A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP1745047A1 (en) | 2007-01-24 |
| MXPA06012231A (es) | 2006-12-15 |
| AR048617A1 (es) | 2006-05-10 |
| AU2005236059A1 (en) | 2005-11-03 |
| PE20060185A1 (es) | 2006-03-20 |
| NZ550591A (en) | 2010-10-29 |
| US20050239795A1 (en) | 2005-10-27 |
| JP2007533754A (ja) | 2007-11-22 |
| EP1745047B1 (en) | 2010-03-24 |
| WO2005103055A1 (en) | 2005-11-03 |
| US7709492B2 (en) | 2010-05-04 |
| AU2005236059B2 (en) | 2009-01-15 |
| ES2342082T3 (es) | 2010-07-01 |
| JP2008231111A (ja) | 2008-10-02 |
| HK1095818A1 (en) | 2007-05-18 |
| CA2563635A1 (en) | 2005-11-03 |
| ATE461932T1 (de) | 2010-04-15 |
| TW200538118A (en) | 2005-12-01 |
| DE602005020127D1 (de) | 2010-05-06 |
| KR20060135901A (ko) | 2006-12-29 |
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